Results 11 to 20 of about 4,006,149 (207)

A highly potent and selective inhibitor Roxyl-WL targeting IDO1 promotes immune response against melanoma

Journal of Enzyme Inhibition and Medicinal Chemistry, 2018
Indoleamine 2,3-dioxygenase 1 (IDO1) activity links to immune escape of cancers. Inhibition of IDO1 provides a new approach for cancer treatment. Most clinical IDO1 drugs show marginal efficacy as single agents.
Guangwei Xu, Tianqi Wang, Yongtao Li, Zhi Huang, Xin Wang, Jianyu Zheng, Shengyong Yang, Yan Fan, Rong Xiang   +8 more
doaj   +3 more sources

Phase I Study of the Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitor Navoximod (GDC-0919) Administered with PD-L1 Inhibitor (Atezolizumab) in Advanced Solid Tumors. [PDF]

Clin Cancer Res, 2019
Purpose: IDO1 induces immune suppression in T cells through l-tryptophan (Trp) depletion and kynurenine (Kyn) accumulation in the local tumor microenvironment, suppressing effector T cells and hyperactivating regulatory T cells (Treg).
Jung KH, LoRusso P, Burris H, Gordon M, Bang YJ, Hellmann MD, Cervantes A, Ochoa de Olza M, Marabelle A, Hodi FS, Ahn MJ, Emens LA, Barlesi F, Hamid O, Calvo E, McDermott D, Soliman H, Rhee I, Lin R, Pourmohamad T, Suchomel J, Tsuhako A, Morrissey K, Mahrus S, Morley R, Pirzkall A, Davis SL.   +26 more
europepmc   +3 more sources

Fragment-based approach to identify IDO1 inhibitor building blocks [PDF]

European Journal of Medicinal Chemistry, 2017
Indoleamine 2,3-dioxygenase 1 (IDO1) is attracting a great deal of interest as drug target in immune-oncology being highly expressed in cancer cells and participating to the tumor immune-editing process.
Ursula Grohmann, Antonio Macchiarulo, Francesco Antonio Greco   +2 more
exaly   +3 more sources

Structure-based optimization of type III indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors

Journal of Enzyme Inhibition and Medicinal Chemistry, 2022
The haem enzyme indoleamine 2,3-dioxygenase 1 (IDO1) catalyses the rate-limiting step in the kynurenine pathway of tryptophan metabolism and plays an essential role in immunity, neuronal function, and ageing. Expression of IDO1 in cancer cells results in
Ute F. Röhrig, Somi Reddy Majjigapu, Pierre Vogel, Aline Reynaud, Florence Pojer, Nahzli Dilek, Patrick Reichenbach, Kelly Ascenção, Melita Irving, George Coukos, Olivier Michielin, Vincent Zoete   +11 more
doaj   +3 more sources

Discovery of Novel 1,2,3-triazole Derivatives as IDO1 Inhibitors

Pharmaceuticals, 2022
Indoleamine 2,3-dioxygenase 1 (IDO1) has received much attention as an immunomodulatory enzyme in the field of cancer immunotherapy. While several IDO1 inhibitors have entered clinical trials, there are currently no IDO1 inhibitor drugs on the market. To
Xixi Hou, Xiaoqing Gong, Longfei Mao, Jie Zhao, Jianxue Yang   +4 more
doaj   +2 more sources

A Novel IDO1/NE Dual Inhibitor, IMM-H018 Prevents the Primary and Secondary Sepsis and Ameliorates the Kidney Injury Through Inhibiting the Cytokine Storm and Microthrombosis, and Reversing Immunosuppression. [PDF]

Adv Sci (Weinh)
IMM‐H018, a dual IDO1/NE inhibitor, demonstrates potent therapeutic efficacy in sepsis by simultaneously targeting excessive inflammation and immune dysfunction. It prevents both primary and secondary sepsis through anti‐inflammatory, immune‐restoring, and renoprotective mechanisms, reducing organ damage, improving immune homeostasis, preserving kidney
Zhou Y, Zhao X, Pan X, Ma Z, Cui H, Wen H, Wang P, Liao X, Qin K, Wang Y, Sheng L, Zhang S.   +11 more
europepmc   +2 more sources

Dual inhibition of IDO1/TDO2 enhances anti-tumor immunity in platinum-resistant non-small cell lung cancer

Cancer & Metabolism, 2023
Background The impact of non-small cell lung cancer (NSCLC) metabolism on the immune microenvironment is not well understood within platinum resistance.
Chunjing Wu, Sydney A. Spector, George Theodoropoulos, Dan J. M. Nguyen, Emily Y. Kim, Ashley Garcia, Niramol Savaraj, Diane C. Lim, Ankita Paul, Lynn G. Feun, Michael Bickerdike, Medhi Wangpaichitr   +11 more
doaj   +2 more sources

INCB24360 (Epacadostat), a Highly Potent and Selective Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitor for Immuno-oncology

ACS Medicinal Chemistry Letters, 2017
A data-centric medicinal chemistry approach led to the invention of a potent and selective IDO1 inhibitor 4f, INCB24360 (epacadostat). The molecular structure of INCB24360 contains several previously unknown or underutilized functional groups in drug ...
Peggy Scherle, Andrew Combs, Richard Wynn   +2 more
exaly   +2 more sources

A selective IDO1 inhibitor, KHK2455, improves efficacy of PD-L1 blockade by modulating both innate and adaptive immunity in a mouse melanoma model [PDF]

Cancer Immunology, Immunotherapy
Indoleamine 2,3-dioxygenase 1 (IDO1) facilitates tumor progression by catabolizing tryptophan into kynurenine (Kyn). While KHK2455, a selective IDO1 inhibitor, reduced Kyn levels in mouse tumors and plasma, it did not exert the expected antitumor ...
Masato Saito, Kana Kunieda, Toshihiko Ishii, Shoko Koshiba, Rui Ohashi, Yutaka Kanda, Takuji Yamada   +6 more
doaj   +2 more sources

The catalytic inhibitor epacadostat can affect the non-enzymatic function of IDO1

Frontiers in Immunology, 2023
Indoleamine 2,3-dioxygenase 1 (IDO1) is a tryptophan metabolizing enzyme chronically activated in many cancer patients and its expression and activity correlate with a poor prognosis.
Maria Laura Belladonna, Maria Teresa Pallotta, Giada Mondanelli   +2 more
exaly   +2 more sources